Pharmacokinetics Flashcards

1
Q

What are the 4 pharmacokinetic processes?

A

ADME

  • Absorption
  • Distribution
  • Metabolism
  • Excretion
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2
Q

What are the 4 pharmacokinetic processes?

A

ADME

  • Absorption
  • Distribution
  • Metabolism
  • Excretion
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3
Q

Polar drugs ____ readily cross the cell membrane

A

CANNOT

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4
Q

Nonpolar drugs _____ readily cross the cell membrane

A

CAN

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5
Q

What are 3 ways for drugs to cross the cell membrane?

A
  1. Facilitated Diffusion - down gradient using channels
  2. Active Transport - requires energy
  3. Simple Diffusion - direct penetration of membrane
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6
Q

What ways for drugs to cross the cell membrane are used mainly for ELIMINATION?

A
  1. Facilitated Diffusion

2. Active Transport

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7
Q

What ways for drugs to cross the cell membrane are used mainly for drugs to REACH their target tissues?

A
  1. Simple Diffusion/direct penetration of the membrane
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8
Q

What is an ex. of an active transporter that is mainly used to eliminate drugs from the cells?

A

P-glycoprotein (MDR1)

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9
Q

The lower the pH, the ___ H+

A

More

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10
Q

In what form can weak acids and weak bases cross cell membranes?

A

UNionized form

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11
Q

Where do weak acids get trapped?

A

Trapped in Basic compartments

- cannot find an H+

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12
Q

Where do weak bases get trapped?

A

Trapped in Acidic compartments

- cannot ditch an H+

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13
Q

If drugs are bound to proteins in the blood, are they active?

A

NO - only active when free

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14
Q

What type of drugs can freely cross the capillary?

A

Lipid-soluble

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15
Q

Polar/Ionized drugs need what types of things in order to leave the capillary?

A

Transporters or pores in the capillary

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16
Q

What is the major route of elimination for drugs?

A

Renal

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17
Q

What are the 3 steps in Renal elimination and what drugs are eliminated?

A
  1. Glomerular filtration - small free drugs
  2. Passive tubular reabsorption - lipid soluble/unionized weak acids and bases
  3. Active tubular secretion - protein bound drugs
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18
Q

As you age, GFR ____

A

Decreases

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19
Q

Mass eliminated per unit time

A

Excretion rate

- will increase as plasma [ ] increases

20
Q

Plasma volume from which all of solute is removed per unit time

A

Clearance

21
Q

Clearance is ____

A

Constant

22
Q

Tachyphylaxis

A

Rapid tolerance

23
Q

Drug physical dependence

A

Tolerance and withdrawal symptoms

24
Q

Drug-Drug interaction

A

1 drug either increases or decreases the effects of the other

25
Q

Idiosyncrasy

A

Unusual response to a drug due to an inherited enzyme defect

26
Q

Teratogenic

A

Drug causes abnormal fetal development

- Characteristic malformations that are dose dependent

27
Q

Adverse drug reactions are more common in what age group?

A

Elderly

28
Q

ex. of a teratogenic drug

A

Thalidomide

- small arms in children

29
Q

Drug-induced carcinogenesis may take years to appear. What drugs have the greatest carcinogenic potential?

A

Cancer chemotherapeutic drugs

30
Q

ex. of a drug that induces carcinogenesis

A

DES (diethylstilbestrol)

- Daughters had increased vaginal and uterine cancers

31
Q

Describe neonates albumin levels and blood brain barrier

A

Neonates albumin level = LOW
- more free and active drug
Neonates BBB = not fully developed
- drugs can freely cross

32
Q

1-2 year old children metabolize drugs _____ than adults

A

FASTER

33
Q

Approximately how many patients will respond to a placebo?

A

1/3

34
Q

Zero-order kinetics

A

CONSTANT amount eliminated per unit time

35
Q

Drug elimination process is saturated in this type of kinetics

A

Zero-order

36
Q

With Zero-order kinetics, amount of drug eliminated is _____ of the drug concentration

A

Independent

37
Q

What is an example of a drug that uses Zero-order kinetics?

A

Ethanol

– Constant amount eliminated per unit time

38
Q

1st-order kinetics

A

Constant FRACTION eliminated per unit time

39
Q

Drug elimination process that is not saturated in this type of kinetics

A

1st-order

40
Q

With 1st-order kinetics, amount of drug eliminated is ____ to the drug concentration

A

Directly related

41
Q

Which type of kinetics is the most common form of drug elimination?

A

1st-order kinetics

42
Q

In 5 half lives, what percentage of the drug will be eliminated?

A

97%

43
Q

Each half life backwards ____ the concentration

A

Doubles

44
Q

Capacity-limited reactions

A

Start as zero-order kinetics and then as concentrations fall transition to 1st-order kinetics

45
Q

Hockey stick like appearance

A

Capacity-limited reactions

46
Q

What is the loading dose?

A

Dose needed to rapidly achieve therapeutic drug concentration for drugs with long half lives

47
Q

What is an example of a drug that needs a loading dose?

A

Digoxin